✦ LIBER ✦

The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity

✍ Scribed by Michael R. Myers; Natalie N. Setzer; Alfred.P. Spada; Paul E. Persons; Cuong Q. Ly; Martin P. Maguire; Allison L. Zulli; Daniel L. Cheney; Asher Zilberstein; Susan E. Johnson; Carol F. Franks; Karen J. Mitchell

Book ID: 104364850
Publisher: Elsevier Science
Year: 1997
Tongue: English
Weight: 211 KB
Volume: 7
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(97)00035-8

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✦ Synopsis

We have identified moderately potent and selective inhibitors ofCSF-1R tyrosine kinase activity, t A preliminary SAR study resulted in the identification of compounds 11 and 20 as the most potent analogues in the series (IC50 = 0.18 jaM). The 3-D-conformation of the 4-(N-alkyl-N-phenyi)-aminoquinazolines has been proposed to be important to the overall selectivity and activity.

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